Name | 2'-deoxy-2'-fluoro-2'-C-methylcytidine |
Synonyms | R1656 R 1656 R-1656 PSI 6130 PSI6130 PSI-6130 PSI 6130 2'-deoxy-2'-fluoro-2'-C-methylcytidine (2'R)-2'-deoxy-2'-fluoro-2'-methyl-Cytidine ethyl 4-broMo-1-Methyl-1H-pyrrole-2-carboxylate 4-Amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyltetrahydrofuran-2-yl)pyr |
CAS | 817204-33-4 |
EINECS | 200-001-2 |
Molecular Formula | C10H14FN3O4 |
Molar Mass | 259.23 |
Density | 1.67 |
Melting Point | 216-218℃ |
Boling Point | 482.4±55.0 °C(Predicted) |
Solubility | DMSO |
Appearance | Solid |
Color | White to Light Brown |
pKa | 12.86±0.70(Predicted) |
Storage Condition | Hygroscopic, -20°C Freezer, Under inert atmosphere |
Stability | Hygroscopic |
Use | PSI-6130 is an HCV NS5B polymerase inhibitor |
In vitro study | PSI-6130 exhibits potent and specific inhibitory activity against HCV RNA replication mediated by the NS5B polymerase. Both PSI-6130 inhibit HCV GT-1b (Con1 strain) and GT-1a (H77 strain) subgenomic RNA replication, with mean EC 50 values of 0.51 and 0.30 μM, respectively. PSI-6130 inhibits 40% human serum with EC 50 of 0.51 μM. PSI-6130 inhibits HCV replication with a mean IC 50 of 0.6 μM, PSI-6130-TP inhibits HCV replicase with a mean IC 50 of 0.34 μM. PSI-6130-TP inhibits recombinant HCV Con1 NS5B on a heteropolymeric RNA template derived from the 3′-end of the negative strand of the HCV genome with an IC 50 of 0.13 μM and K i of 0.023 μM. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.858 ml | 19.288 ml | 38.576 ml |
5 mM | 0.772 ml | 3.858 ml | 7.715 ml |
10 mM | 0.386 ml | 1.929 ml | 3.858 ml |
5 mM | 0.077 ml | 0.386 ml | 0.772 ml |
biological activity | PSI-6130 is a highly effective, selective HCV NS5B polymerase inhibitor, which can inhibit HCV replication with an IC50 value of 0.6 μM. |
target | IC50: 0.6 μM (HCV replication) |
in vitro study | PSI-6130 exhibits potent and specific inhibitory activity against HCV RNA replication mediated by the NS5B polymerase. Both PSI-6130 inhibit HCV GT-1b (Con1 STRAIN) and GT-1a (H77 STRAIN) subgenomic RNA replication, with mean EC 50 values of 0.51 and 0.30 μM, respectively. PSI-6130 inhibits 40% human serum with EC 50 of 0.51 μ m. PSI-6130 inhibits HCV replication with a mean IC 50 of 0.6 μ m, PSI-6130-TP inhibits HCV replicase with a mean IC 50 of 0.34 μ m. PSI-6130-TP inhibits recombinant HCV Con1 NS5B on a heteropolymeric RNA template derived from the 3 '-end of the negative strand of the HCV local with an IC 50 of 0.13 μ m and K I of 0.023 μ m. |